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GPR31
G-protein coupled receptor 31 also known as 12-(S)-HETE receptor is a protein that in humans is encoded by the ''GPR31'' gene. The human gene is located on chromosome 6q27 and encodes a G-protein coupled receptor protein composed of 319 amino acids.〔(【引用サイトリンク】 url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=2853 )〕
== Function ==
The GPR31 receptor is most closely related in amino acid sequence to the oxoeicosanoid receptor 1, a G-protein coupled receptor encoded by the GPR170 gene. Oxoeicosanoid receptor 1 is the receptor for a family of arachidonic acid metabolites made by 5-lipoxygenase viz., 5-Hydroxyicosatetraenoic acid (5-HETE), 5-oxoicosanoic acid (5-oxo-ETE) and other members of this family of broadly bioactive cell stimuli. The GPR31 receptor is a receptor for very different arachidonic acid metabolite, 12-hydroxyeicosatetraenoic acid (12-HETE), whose synthesis is catalyzed by 12-lipoxygenase; this conclusion is based on studies that cloned the receptor from the PC-3 prostate cancer cell line and found that the cloned receptor, when expressed in other cell types, bound with high affinity (Kd=5 nM) and mediated the actions of low concentrations of the ''S'' but not ''R'' stereoisomer of 12-HETE.〔 In a ()GTPγS binding assay, which indirectly estimates a receptor's binding affinity with a ligand by measuring this ligand's ability to stimulate the receptor to bind ()GTPγS, 12(''S'')-HETE stimulated the cloned GPR31 receptor to bind ()GTPγS with an EC50 (effective concentration causing a 50% of maximal rise in ()GTPγS binding) was <0.3 nM; it was 42 nm for 15(''S'')-HETE, 390 nM for 5(''S'')-HETE, and undetectable for 12(''R'')-HETE.〔J Biol Chem. 2011 Sep 30;286(39):33832-40. doi: 10.1074/jbc.M110.216564〕 Importantly, however, we do not known if GPR31 interacts with structural analogs of 12(''S'')-HETE such as 12-oxo-ETE (a metabolite of 12(''S'')-HETE), various 5,12-diHETEs including LTB4, and an array of bioactive 12(''S'')-HETE and 12(''R'')-HETE metabolites, the Hepoxilins. Further studies will be needed to determine if the GPR31 receptor is dedicated to binding and mediating the aciont of 12(''S'')-HETE more or less exclusively or, like the oxoeicosanoid receptor 1, binds and mediates the actions of a family of analogs.
GPR31 receptor, like the oxoeicosanoid receptor, activates the MEK-ERK1/2 pathway of intercellular signaling but unlike the oxoeicoanaoid receptor does not trigger rises in the concentration of cytosolic Ca2+; it also activates NFκB.〔 GPR31 receptor therefore exhibits the stereospecificity and some other features generally expected from a true GPR receptor.
12(''S'')-HETE also: a) binds to and activates the leukotriene B4 receptor-2 (BLT2), a G protein-coupled receptor for the 5-lipoxygenase-derived arachidonic acid metabolite, LTB4 and LTB4 metabolites;〔 b) binds to, but rather than activating, inhibits the G protein-coupled receptor for the cyclooxygenase-derived arachidonic acid metabolites prostaglandin H2 and thromboxane A2; c) binds with high affinity to a 50 kilodalton (Kda) subunit of a 650 kDa cytosolic and nuclear protein complex; and d) binds with low affinity to and activates intracellular Peroxisome proliferator-activated receptor gamma. These alternate binding and cell-activating sites complicate the determination of 12(''S'')-HETE's dependency on GPR31 in stimulating cells as well as the overall functoin of GPR31. The effects of GPR31 Gene knockout in animal models, a technique critical to defining the in vivo function of genes, will be critical to shedding light on these issues.
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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